Design and synthesis of substituted N-(1, 3-diphenyl-1H-pyrazol-5-yl) benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5

…, J Cao, AL Rodriguez, PJ Conn, AH Newman

文献索引：Zou, Mu-Fa; Cao, Jianjing; Rodriguez, Alice L.; Jeffrey Conn; Newman, Amy Hauck Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 9 p. 2650 - 2654

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被引用次数: 13

摘要

Based on SAR in the alkyne class of mGlu5 receptor negative allosteric modulators and a set of amide-based positive allosteric modulators, optimized substitution of the aryl 'b'ring was used to create substituted N-(1, 3-diphenyl-1H-pyrazol-5-yl) benzamides. Results from an mGlu5 receptor functional assay, using calcium fluorescence, revealed varying efficacies and potencies that provide evidence that subtle changes in compounds within a close ...